Romanian Society of Pharmaceutical Sciences
 

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MOLECULAR DETERMINANTS OF SOLUBILITY IN BIORELEVANT FLUIDS FOR DIBENZOTHIEPINE COMPOUNDS

CAMELIA ELENA STECOZA1, DRAGOŞ CIOLAN1, FLAVIAN ŞTEFAN RĂDULESCU2*, GEORGE MIHAI NIŢULESCU1, MAGDALENA MAJEKOVA4, DALIA SIMONA MIRON3

University of Medicine and Pharmacy „Carol Davila” Bucharest, Faculty of Pharmacy, 6 Traian Vuia street, 020956, Bucharest, Romania
1 Department of Pharmaceutical Chemistry
2 Department of Drug Industry and Pharmaceutical Biotechnologies
3 Department of Pharmaceutical Physics and Informatics
4 Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dubravska cesta 9, 84104, Bratislava, Slovakia

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The solubility profile of ten benzothiepine compounds was screened using the currently recommended fasted and fed state simulated gastric and intestinal fluids, as part of the in vitro evaluation of their biopharmaceutical properties and of the developability potential. The experimental data was compared with the previously reported in silico predictions generated on ADMET Predictor platform. The results indicated a considerable impact of the endogenous tensioactives, with maximum absorbable doses varying between 20 and 200 mg. The non-correlation between the in vitro evaluated and in silico estimates were significant, especially for the gastric media. The global solubility profile seems to indicate that the evaluated compounds have dissolution-rate limited characteristics and belong to the sub-class IIa of the Biopharmaceutical Classification System.